Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
  • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/66—Phosphorus compounds

Definitions

• the present invention relates to active ingredient combinations with antibiotic properties, their production and use and pharmaceutical preparations based on them.
• lower alkyl means straight or branched chain alkyl radicals having preferably up to 8 carbon atoms, such as ethyl, propyl, butyl, tert-butyl, pentyl and hexyl.
• hydroxy lower alkyl groups are hydroxyethyl, 3-hydroxypropyl and 4-hydroxybutyl.
• halogen includes fluorine, chlorine, bromine and iodine; Examples of halomethyl groups are chloromethyl, dichloromethyl and trifluoromethyl.
• the in vitro activity of the combinations according to the invention can also be shown by the microtiter checkerboard method.
• This method produces filter-sterilized basic solutions of compounds I and a nocardicin antibiotic that are 4.8 times as concentrated as the solutions to be tested. Aliquots of the culture medium (50 ⁇ l) were added to all 12 (1-12) x 8 (A- H ) holes on the microtiter plate, except for hole 12H. 50 ⁇ l of the peptide solution was then added to each hole in the twelfth row and 100 ⁇ l to hole 12H.
• the peptide-containing solutions were then diluted within the series AH by transferring 50 .mu.l from series 12 to series 11, mixing well, and again transferring 50 .mu.l to series 10 and repeating this procedure up to series 2, see above that row 1 was left out. Then 50 ⁇ l of a solution of a nocardicin antibiotic was added to each hole in row H and also diluted in the manner described above within rows 1-12, the last hole in each row again being omitted. After the volumes were brought up to 100 .mu.l by adding 50 .mu.l of nutrient liquid, 20 .mu.l of a 1/1000 dilution of an overnight culture was subjected to a test organism added.
• the active substance combinations according to the invention can be administered in the form of pharmaceutical preparations which are also the subject of the present invention.
• the usual pharmaceutical carriers compatible with the compounds of formula 1 or their salts and the nocardicin antibiotics are suitable for the preparation of the preparations.
• Carrier materials can be liquid or solid, organic or inorganic in nature and include, for example, water, gelatin, mannitol, mineral oils, vegetable oils, gum arabic, propylene glycols or polyalkylene glycols.
• the pharmaceutical preparations can be produced in a manner known per se, for example by mixing the individual components with the suitable carrier materials and bringing them into a suitable pharmaceutical form.
• the pharmaceutical preparations can be in solid form (for example as lyophilisates) or in liquid form (for example as solutions, suspensions or emulsions). If necessary, they are sterilized and / or contain further auxiliaries such as preservatives, stabilizers, wetting agents or emulsifiers, agents for improving the taste, salts for changing the osmotic Pressure or buffer substances. When using buffers, the pH of the preparations can vary within the usual limits.
• the content of the active compound combinations according to the invention in pharmaceutical preparations can vary within wide limits.
• the optimal daily dose depends on the components actually used, the route of administration, the type of infection, etc.
• the daily dose in the case of parenteral administration is approximately 200-2000 mg of the mixture of the active components.
• This dose can be administered as a single dose or in partial doses and can be increased or decreased in special situations depending on the doctor's prescription based on individual requirements.
• Lyophilisate for the production of injection solutions containing the following ingredients:
• a solution for injection is prepared by dissolving 100 ml of nocardicin A sodium salt in 1 ml of a solution containing 100 mg (1R) -1- (L-norvalylamino) ethylphosphonic acid per ml of a suitable buffer.
• a suitable buffer can be composed as follows:
• a powdery mixture for the production of injection solutions can have the following composition:
• This mixture is prepared in a manner analogous to Example 1. To prepare a solution for injection, the mixture is dissolved in 2 ml of water for injections.
• the mixture is prepared in a manner analogous to Example 1. To prepare a solution for injection, the mixture is dissolved in 2 ml of water for injections.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Chemistry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Seeds, Soups, And Other Foods (AREA)

Applications Claiming Priority (4)

Publications (1)

Family

ID=26273034

Family Applications (1)

Country Status (10)

Citations (3)

• 1980
  • 1980-09-19 FI FI802964A patent/FI802964A7/fi not_active Application Discontinuation
  • 1980-09-19 EP EP80105636A patent/EP0026410A1/de not_active Withdrawn
  • 1980-09-24 IL IL61135A patent/IL61135A0/xx unknown
  • 1980-09-26 GR GR62971A patent/GR70015B/el unknown
  • 1980-09-26 NO NO802858A patent/NO802858L/no unknown
  • 1980-09-26 PT PT71846A patent/PT71846B/pt unknown
  • 1980-09-26 DK DK409680A patent/DK409680A/da unknown
  • 1980-09-27 KR KR1019800003764A patent/KR830004325A/ko not_active Withdrawn
  • 1980-09-29 MC MC801472A patent/MC1349A1/fr unknown
  • 1980-09-29 AU AU62781/80A patent/AU6278180A/en not_active Abandoned

Patent Citations (3)

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